| 中文名称 |
Mizagliflozin
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| 英文名称 |
Mizagliflozin
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| 英文别名 |
Mizagliflozin;1X96A704XV;3-((3-(4-((5-isopropyl-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-1H-pyrazol-4-yl)methyl)-3-methylphenoxy)propyl)amino)-2,2-dimethylpropanamide;Mizagliflozin [INN];Mizagliflozin [WHO-DD];GTPL9547;s8939;Q27253060;2,2-dimethyl-3-[3-[3-methyl-4-[[3-propan-2-yl-5-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-2H-pyrazol-4-yl]methyl]phen
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| Cas No. |
666843-10-3
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| 分子式 |
C28H44N4O8
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| 分子量 |
564.67
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| 包装储存 |
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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| 详情描述 |
Mizagliflozin (DSP-3235 free base) 是一种高效、口服、选择性的 SGLT1 抑制剂,对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 的对 SGLT1 选择性是 SGLT2 的 303 倍。Mizagliflozin 是一种抗糖尿病药物,可以改善餐后血糖波动。Mizagliflozin 在改善慢性便秘方面具有潜在的作用。
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| 产品详情 |
Mizagliflozin (DSP-3235 free base) 是一种高效、口服、选择性的 SGLT1 抑制剂,对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 的对 SGLT1 选择性是 SGLT2 的 303 倍。Mizagliflozin 是一种抗糖尿病药物,可以改善餐后血糖波动。Mizagliflozin 在改善慢性便秘方面具有潜在的作用。
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| 生物活性 |
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a K i of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
Ki: 27 nM (hSGLT1), 8170 nM (hSGLT2)
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| 体内研究(In Vivo) |
Mizagliflozin (DSP-3235 free base) (3-30 mg/kg; oral) exerts a laxative effect.
Mizagliflozin administrated intravenously (0.3?mg/kg) and orally (3?mg/kg) declined with a short half-life (0.23 and 1.14?h, respectively) has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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| ClinicalTrial |
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| 参考文献 |
[1]. Inoue T, et al. Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation. Eur J Pharmacol. 2017 Jul 5;806:25-31.[2]. Ohno H, et al. Absorption, disposition, metabolism and excretion of [14C]mizagliflozin, a novel selective SGLT1 inhibitor, in rats. Xenobiotica. 2019 Apr;49(4):463-473.
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| 溶解度数据 |
In Vitro: H2O : ≥ 100 mg/mL (177.09 mM)DMSO : 100 mg/mL (177.09 mM; Need ultrasonic)
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[1]. Inoue T, et al. Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation. Eur J Pharmacol. 2017 Jul 5;806:25-31.[2]. Ohno H, et al. Absorption, disposition, metabolism and excretion of [14C]mizagliflozin, a novel selective SGLT1 inhibitor, in rats. Xenobiotica. 2019 Apr;49(4):463-473.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。